Article
Gatekeeper mutations mediate resistance to BRAF-targeted therapies.
Science translational medicine - 9 Jun 2010
Whittaker Steven, Kirk Ruth, Hayward Robert, Zambon Alfonso, Viros Amaya, Cantarino Neus, Affolter Annette, Nourry Arnaud, Niculescu-Duvaz Dan, Springer Caroline, Marais Richard
Abstract excerpt
BRAF is a serine-threonine-specific protein kinase that is mutated in 2% of human cancers. Oncogenic BRAF is a validated therapeutic target that constitutively activates mitogen-activated protein kinase kinase (MEK)-extracellular signal-regulated kinase (ERK) signaling, driving tumor cell proliferation and survival. Drugs designed to target BRAF have been developed, but it is difficult to prove that they mediate...
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